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Prodrugs of cephalosporin RWJ-333441 (MC-04,546) with improved aqueous solubility. | LitMetric
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Prodrugs of cephalosporin RWJ-333441 (MC-04,546) with improved aqueous solubility.

Scott J Hecker Trevor Calkins Mary E Price Keith Huie Sharon Chen Tomasz W Glinka Michael N Dudley

Antimicrob Agents Chemother

Microcide Pharmaceuticals, Inc., Mountain View, California, USA.

Published: June 2003

To improve the aqueous solubility of anti-methicillin-resistant Staphylococcus aureus cephalosporin RWJ-333441 for parenteral administration, acyl derivatives of the C-3 primary amino group were prepared and evaluated for solubility, cleavage in serum in vitro, and conversion to RWJ-333441 in vivo. Improved solubility at physiologic pH values and release of RWJ-333441 in vitro and in vivo were observed for several prodrugs, including the aspartate derivative RWJ-333442.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC155843PMC
http://dx.doi.org/10.1128/AAC.47.6.2043-2046.2003DOI Listing

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